KinasePro

Kinase Chemistry – Just a year and a half behind the times.

Archive for the ‘Cephalon’ Category

Ceph ‘n’ PCOP got C-Met

Posted by kinasepro on August 21, 2008

The 15M Pharmacopeia and Cephalon deal from a couple years ago was likely for compounds like these c-Met / Alk inhibitors:

O=C(NC)C1=CC=CC(F)=C1NC2=NC(NC3=CC=C4C(C)(C)CC(NCCOC)CNC4=C3)=NC=C2Cl

O=C(NC)C1=CC=CC(F)=C1NC2=NC(NC3=CC=C4C(C)(C)CC(NCCOC)CNC4=C3)=NC=C2Cl

WO/2008/051547

yeh, its 1300 pages and I know they’re old, but I got some catching up to do…

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Posted in c-Met, Cephalon, Pharmacopeia | Leave a Comment »

At least its free…

Posted by kinasepro on August 20, 2008

The new ‘Perspective‘: Some useful information bracketed by useless commentary.

Affinity is not even a check-box on the road to an approved drug.  What’s stopping 99.9% of real compounds coming from real programs isn’t potency.  This makes a discussion of how many hydrogen bonds to the hinge are in approved drugs totally irrelevant.

Fact Check:

>> Ruboxistaurin is not an approved drug.

>> Fasudil is only approved in Japan.

>> And you forgot Tasigna

Posted in Cephalon, General Interest | Leave a Comment »

A-[CEP-701]

Posted by kinasepro on June 25, 2007

So, what’s Abbott doing making solid forms of Lestaurtinib?

WO/2007/070444, US20070135628, US20070135401

Oh, and CC pointed out that CEP-701 / lestaurtinib is claimed to be in Ph3 trials for AML, so add that one to the list, I guess. I can’t find the trial in the US or EU databases, so may be in Asia?

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Lestaurtinib

Posted by kinasepro on May 28, 2007

O=C1NCC2=C1C3=C4N([C@H]5C[C@](O)([C@](C)(N6C4=C2C7=C6C=CC=C7)O5)CO)C8=C3C=CC=C8

Lestaurtinib / CEP-701 is currently in trials for a handful of indications and first appeared in WO/1988/07045 (US,4,923,986) via Kyowa Hakko Kogyo. The series was first described as a group of PKC inhibitors, but later came this ’98 press release: (emphasis mine)

CEP-701 is one of a series of specific receptor trk kinase inhibitor derived from the indolocarbazole K252a, which was originally synthesized by Kyowa Hakko Kogyo Co., Ltd., Tokyo, Japan

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Posted in c-Met, Cephalon, Flt3, JAK, Trk, VEGF | 3 Comments »